Physico Chemical Methods In Drug Discovery And Development
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Physico Chemical Methods In Drug Discovery And Development
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Author : Zoran Mandic
language : en
Publisher: IAPC Publishing
Release Date : 2012
Physico Chemical Methods In Drug Discovery And Development written by Zoran Mandic and has been published by IAPC Publishing this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012 with categories.
Physico Chemical And Computational Approaches To Drug Discovery
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Author : Javier Luque
language : en
Publisher: Royal Society of Chemistry
Release Date : 2012
Physico Chemical And Computational Approaches To Drug Discovery written by Javier Luque and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012 with Medical categories.
This title covers a wide range of topics relevant to the development of drugs. It provides a comprehensive description of the major methodological strategies available for rational drug discovery.
Discovering And Developing Molecules With Optimal Drug Like Properties
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Author : Allen C Templeton
language : en
Publisher: Springer
Release Date : 2014-10-31
Discovering And Developing Molecules With Optimal Drug Like Properties written by Allen C Templeton and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2014-10-31 with Medical categories.
This authoritative volume provides a contemporary view on the latest research in molecules with optimal drug-like properties. It is a valuable source to access current best practices as well as new research techniques and strategies. Written by leading scientists in their fields, the text consists of fourteen chapters with an underlying theme of early collaborative opportunities between pharmaceutical and discovery sciences. The book explores the practical realities of performing physical pharmaceutical and biopharmaceutical research in the context of drug discovery with short timelines and low compound availability. Chapters cover strategies and tactics to enable discovery as well as predictive approaches to establish, understand and communicate risks in early development. It also examines the detection, characterization, and assessment of risks on the solid state properties of advanced discovery and early development candidates, highlighting the link between solid state properties and critical development parameters such as solubility and stability. Final chapters center on techniques to improve molecular solubilization and prevent precipitation, with particularly emphasis on linking physiochemical properties of molecules to formulation selection in preclinical and clinical settings.
Modern Methods Of Drug Discovery
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Author : Alexander Hillisch
language : en
Publisher: Birkhäuser
Release Date : 2012-11-28
Modern Methods Of Drug Discovery written by Alexander Hillisch and has been published by Birkhäuser this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-11-28 with Medical categories.
Research in the pharmaceutical industry today is in many respects quite different from what it used to be only fifteen years ago. There have been dramatic changes in approaches for identifying new chemical entities with a desired biological activity. While chemical modification of existing leads was the most important approach in the 1970s and 1980s, high-throughput screening and structure-based design are now major players among a multitude of methods used in drug discov ery. Quite often, companies favor one of these relatively new approaches over the other, e.g., screening over rational design, or vice versa, but we believe that an intelligent and concerted use of several or all methods currently available to drug discovery will be more successful in the medium term. What has changed most significantly in the past few years is the time available for identifying new chemical entities. Because of the high costs of drug discovery projects, pressure for maximum success in the shortest possible time is higher than ever. In addition, the multidisciplinary character of the field is much more pronounced today than it used to be. As a consequence, researchers and project managers in the pharmaceutical industry should have a solid knowledge of the more important methods available to drug discovery, because it is the rapidly and intelligently combined use of these which will determine the success or failure of preclinical projects.
Absorption And Drug Development
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Author : Alex Avdeef
language : en
Publisher: John Wiley & Sons
Release Date : 2012-05-22
Absorption And Drug Development written by Alex Avdeef and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-05-22 with Medical categories.
Explains how to perform and analyze the results of the latest physicochemical methods With this book as their guide, readers have access to all the current information needed to thoroughly investigate and accurately determine a compound's pharmaceutical properties and their effects on drug absorption. The book emphasizes oral absorption, explaining all the physicochemical methods used today to analyze drug candidates. Moreover, the author provides expert guidance to help readers analyze the results of their studies in order to select the most promising drug candidates. This Second Edition has been thoroughly updated and revised, incorporating all the latest research findings, methods, and resources, including: Descriptions and applications of new PAMPA models, drawing on more than thirty papers published by the author's research group Two new chapters examining permeability and Caco-2/MDCK and permeability and the blood-brain barrier Expanded information and methods to support pKa determination New examples explaining the treatment of practically insoluble test compounds Additional case studies demonstrating the use of the latest physicochemical techniques New, revised, and expanded database tables throughout the book Well over 200 drawings help readers better understand difficult concepts and provide a visual guide to complex procedures. In addition, over 800 references serve as a gateway to the primary literature in the field, facilitating further research into all the topics covered in the book. This Second Edition is recommended as a reference for researchers in pharmaceutical R&D as well as in agrochemical, environmental, and other related areas of research. It is also recommended as a supplemental text for graduate courses in pharmaceutics.
Physicochemical And Biomimetic Properties In Drug Discovery
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Author : Klara Valko
language : en
Publisher: John Wiley & Sons
Release Date : 2013-11-25
Physicochemical And Biomimetic Properties In Drug Discovery written by Klara Valko and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-11-25 with Medical categories.
Demonstrating how and why to measure physicochemical and biomimetic properties in early stages of drug discovery for lead optimization, Physicochemical and Biomimetic Properties in Drug Discovery encourages readers to discover relationships between various measurements and develop a sense of interdisciplinary thinking that will add to new research in drug discovery. This practical guide includes detailed descriptions of state-of-the-art chromatographic techniques and uses real-life examples and models to help medicinal chemists and scientists and advanced graduate students apply measurement data for optimal drug discovery.
Successful Drug Discovery
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Author : János Fischer
language : en
Publisher: John Wiley & Sons
Release Date : 2019-07-13
Successful Drug Discovery written by János Fischer and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-07-13 with Medical categories.
Provides unique insider insight into the current drug development process, and what it takes to achieve success In this fourth volume in the series, inventors and primary developers of drugs that made it to the market continue telling the story of the drugs? discovery and development, and discuss the sometimes twisted route from the first drug candidate molecule to the final marketed one. Beginning with a general section addressing overarching topics for drug discovery, the book offers seven chapters that feature selected case studies describing recently introduced drugs or drug classes. These include small molecule drugs as well as biopharmaceuticals and range across different therapeutic fields. Together, they provide a representative cross-section of the present-day drug development effort. Successful Drug Discovery: Volume 4 covers trends in peptide-based drug discovery and the physicochemical properties of recently approved oral drugs. The section on drug class studies looks at antibody-drug conjugates and the discovery, evolution, and therapeutic potential of dopamine partial agonists. Featured case studies examine the discovery of Etelcalcetide for the treatment of secondary hyper-parathyroidism in patients with chronic kidney disease; the development of Lenvatinib Mesylate; the discovery and development of Venetoclax; and more. -Focuses on recently introduced drugs that have not been featured in any textbooks or general references, including Ocrelizumab, a new generation of anti-CD-20 mAb for the treatment of multiple sclerosis, and Venetoclax, a selective antagonist of BCL-2 -Features personal experiences of successful drug developers from industry and academia -Endorsed and supported by the International Union of Pure and Applied Chemistry (IUPAC) Successful Drug Discovery: Volume 4 provides a fascinating and informative look into the process of drug discovery and would be a great reference for those in the pharmaceutical industry, organic and pharmaceutical chemists, and lecturers in pharmacy.
Optimization In Drug Discovery
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Author : Zhengyin Yan
language : en
Publisher: Humana Press
Release Date : 2004-08-11
Optimization In Drug Discovery written by Zhengyin Yan and has been published by Humana Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2004-08-11 with Medical categories.
Recent analyses of drug attrition rates reveal that a significant number of drug candidates fail in the later stage of clinical development owing to absorption, distribution, metabolism, elimination (ADME), and toxicity issues. Lead optimization in drug discovery, a process attempting to uncover and correct these defects of drug candidates, is highly beneficial in lowering the cost and time to develop therapeutic drugs by reducing drug candidate failures in development. At present, parallel synthesis combining with high-throughput screening has made it easier to generate highly potent compounds (i. e. , hits). However, to be a potential drug, a hit must have drug-like characteristics in addition to potency, which include optimal physicochemical properties, reasonable ph- macokinetic parameters, and good safety profiles. Therefore, research tools must be available in drug discovery to rapidly screen for compounds with favorable drug-like properties, and thus adequate resources can be directed to projects with high potential. Optimization in Drug Discovery: In Vitro Methods is a compilation of detailed experimental protocols necessary for setting up a variety of assays important in compound evaluation. A total of 25 chapters, contributed by many experts in their research areas, cover a wide spectrum of subjects including physicochemical properties, abso- tion, plasma binding, metabolism, drug interactions, and toxicity. A good pharmacokinetic profile has long been recognized as an imp- tant drug-like characteristic. Pharmacokinetic parameters are affected by many properties of drug molecules such as physicochemical nature, abso- tion, metabolic stability, and so on.
Admet For Medicinal Chemists
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Author : Katya Tsaioun
language : en
Publisher: John Wiley & Sons
Release Date : 2011-02-15
Admet For Medicinal Chemists written by Katya Tsaioun and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2011-02-15 with Medical categories.
This book guides medicinal chemists in how to implement early ADMET testing in their workflow in order to improve both the speed and efficiency of their efforts. Although many pharmaceutical companies have dedicated groups directly interfacing with drug discovery, the scientific principles and strategies are practiced in a variety of different ways. This book answers the need to regularize the drug discovery interface; it defines and reviews the field of ADME for medicinal chemists. In addition, the scientific principles and the tools utilized by ADME scientists in a discovery setting, as applied to medicinal chemistry and structure modification to improve drug-like properties of drug candidates, are examined.
Lead Seeking Approaches
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Author : Matthew M. Hayward
language : en
Publisher: Springer Science & Business Media
Release Date : 2010-03-12
Lead Seeking Approaches written by Matthew M. Hayward and has been published by Springer Science & Business Media this book supported file pdf, txt, epub, kindle and other format this book has been release on 2010-03-12 with Science categories.
High quality leads provide the foundation for the discovery of successful clinical development candidates, and therefore the identi?cation of leads is an essential part of drug discovery. The process for the identi?cation of leads generally starts with the screening of a compound collection, either an HTS of a relatively large compound collection (hundreds of thousands to one million plus compounds) or a more focused screen of a smaller set of compounds that have been preselected for the target of interest. Virtual screening methods such as structure-based or pharmacophore-based searches can complement or replace one of the above approaches. Once hits are identi?ed from one or more of these screening methods, they need to be thoroughly characterized in order to con?rm activity and identify areas in need of optimization. Finally, once fully characterized hits are identi?ed, preliminary optimization through synthetic modi?cation is carried out to generate leads. Parallel optimization of all properties, including biological, physicochemical, and ADME is the most ef?cient approach to the identi?cation of leads. Hit characterization is described in the previous chapter. The focus of this chapter is on hit optimization and the identi?- tion of leads. After a general overview of these processes, examples taken from the literature since 2001 will be used to illustrate speci?c points. There are also a number of excellent reviews covering the lead identi?cation process [1–6].